CN101605543A - 具有校正突变-cftr加工活性的化合物及其应用 - Google Patents

具有校正突变-cftr加工活性的化合物及其应用 Download PDF

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Publication number
CN101605543A
CN101605543A CNA2006800150356A CN200680015035A CN101605543A CN 101605543 A CN101605543 A CN 101605543A CN A2006800150356 A CNA2006800150356 A CN A2006800150356A CN 200680015035 A CN200680015035 A CN 200680015035A CN 101605543 A CN101605543 A CN 101605543A
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pharmaceutical composition
phenyl
cftr
pharmaceutically acceptable
chemical compound
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Chinese (zh)
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A·弗克曼
N·佩德蒙特
L·J·V·加里耶塔
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University of California
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University of California
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
CNA2006800150356A 2005-03-18 2006-03-08 具有校正突变-cftr加工活性的化合物及其应用 Pending CN101605543A (zh)

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US66350105P 2005-03-18 2005-03-18
US60/663,501 2005-03-18

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CN101605543A true CN101605543A (zh) 2009-12-16

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US (1) US8143295B2 (US20080318984A1-20081225-C00062.png)
EP (1) EP1863522A4 (US20080318984A1-20081225-C00062.png)
JP (1) JP2008538107A (US20080318984A1-20081225-C00062.png)
KR (1) KR20070114820A (US20080318984A1-20081225-C00062.png)
CN (1) CN101605543A (US20080318984A1-20081225-C00062.png)
AU (1) AU2006227833A1 (US20080318984A1-20081225-C00062.png)
BR (1) BRPI0608453A2 (US20080318984A1-20081225-C00062.png)
CA (1) CA2600869A1 (US20080318984A1-20081225-C00062.png)
IL (1) IL185999A0 (US20080318984A1-20081225-C00062.png)
MX (1) MX2007011512A (US20080318984A1-20081225-C00062.png)
RU (1) RU2007138584A (US20080318984A1-20081225-C00062.png)
WO (1) WO2006101740A2 (US20080318984A1-20081225-C00062.png)

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CN102892764A (zh) * 2010-03-25 2013-01-23 弗特克斯药品有限公司 (r)-1(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(1-(2,3-二羟基丙基)-6-氟-2-(1-羟基-2-甲基丙-2-基)-1h-吲哚-5-基)环丙烷甲酰胺的固体形式
US9732080B2 (en) 2006-11-03 2017-08-15 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US9758510B2 (en) 2006-04-07 2017-09-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9974781B2 (en) 2006-04-07 2018-05-22 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CN108463223A (zh) * 2015-10-09 2018-08-28 艾伯维公司 用于治疗囊性纤维化的增效剂-校正剂组合
US10058546B2 (en) 2012-07-16 2018-08-28 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxo1-5-y1)-N-(1-(2,3-dihydroxypropy1)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-y1)-1H-indol-5-y1) cyclopropanecarbox-amide and administration thereof
US10071979B2 (en) 2010-04-22 2018-09-11 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
US10081621B2 (en) 2010-03-25 2018-09-25 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
US10206877B2 (en) 2014-04-15 2019-02-19 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases

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CA2635214A1 (en) * 2005-12-27 2007-07-05 Vertex Pharmaceuticals Incorporated Compounds useful in cftr assays and methods therewith
BRPI0620960A2 (pt) 2005-12-28 2011-11-29 Vertex Pharmaceuticals Incorporated formas sólidas de n-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-didro-4- oxiquinolina-3- carboxamida
CN101096363B (zh) * 2006-06-27 2011-05-11 中国人民解放军军事医学科学院毒物药物研究所 2,4,5-三取代噻唑类化合物、其制备方法、药物组合物及其制药用途
KR20100016073A (ko) 2007-04-02 2010-02-12 인스티튜트 포 원월드 헬스 Cftr 억제제 화합물 및 이의 용도
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WO2009023509A2 (en) * 2007-08-09 2009-02-19 Vertex Pharmaceuticals Incorporated Therapeutic combinations useful in treating cftr related diseases
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US8389736B2 (en) * 2007-10-16 2013-03-05 The Regents Of The University Of California Compounds having activity in correcting mutant-CFTR processing and uses thereof
PL2578571T3 (pl) 2007-11-16 2016-03-31 Vertex Pharma Modulatory izochinolinowe transporterów zawierających kasetę wiążącą ATP
SI2225230T1 (sl) 2007-12-07 2017-03-31 Vertex Pharmaceuticals Incorporated Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline
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KR101955863B1 (ko) 2009-03-20 2019-03-07 버텍스 파마슈티칼스 인코포레이티드 낭성 섬유증 막횡단 전도도 조절자의 조정자의 제조 방법
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US10253020B2 (en) 2009-06-12 2019-04-09 Abivax Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging
US20110098311A1 (en) 2009-10-22 2011-04-28 Vertex Pharmaceuticals Incorported Compositions for treatment of cystic fibrosis and other chronic diseases
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US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
JP2013536231A (ja) 2010-08-23 2013-09-19 バーテックス ファーマシューティカルズ インコーポレイテッド (r)−1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)−n−(1−(2,3−ジヒドロキシプロピル)−6−フルオロ−2−(1−ヒドロキシ−2−メチルプロパン−2−イル)−1h−インドール−5−イル)シクロプロパンカルボキサミドを含む医薬組成物およびその投与
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US10239867B2 (en) 2006-04-07 2019-03-26 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US11639347B2 (en) 2006-04-07 2023-05-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9758510B2 (en) 2006-04-07 2017-09-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9974781B2 (en) 2006-04-07 2018-05-22 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10987348B2 (en) 2006-04-07 2021-04-27 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10975061B2 (en) 2006-04-07 2021-04-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US9732080B2 (en) 2006-11-03 2017-08-15 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US10906891B2 (en) 2010-03-25 2021-02-02 Vertex Pharmaceuticals Incoporated Solid forms of (R)-1(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
US10081621B2 (en) 2010-03-25 2018-09-25 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
CN102892764A (zh) * 2010-03-25 2013-01-23 弗特克斯药品有限公司 (r)-1(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(1-(2,3-二羟基丙基)-6-氟-2-(1-羟基-2-甲基丙-2-基)-1h-吲哚-5-基)环丙烷甲酰胺的固体形式
US11578062B2 (en) 2010-03-25 2023-02-14 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
CN102892764B (zh) * 2010-03-25 2016-07-06 弗特克斯药品有限公司 (r)-1(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(1-(2,3-二羟基丙基)-6-氟-2-(1-羟基-2-甲基丙-2-基)-1h-吲哚-5-基)环丙烷甲酰胺的固体形式
US10071979B2 (en) 2010-04-22 2018-09-11 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
US10058546B2 (en) 2012-07-16 2018-08-28 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-difluorobenzo[D][1,3]dioxo1-5-y1)-N-(1-(2,3-dihydroxypropy1)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-y1)-1H-indol-5-y1) cyclopropanecarbox-amide and administration thereof
US10206877B2 (en) 2014-04-15 2019-02-19 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US10980746B2 (en) 2014-04-15 2021-04-20 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US11951212B2 (en) 2014-04-15 2024-04-09 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
CN108463223A (zh) * 2015-10-09 2018-08-28 艾伯维公司 用于治疗囊性纤维化的增效剂-校正剂组合

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EP1863522A4 (en) 2010-11-10
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US20080318984A1 (en) 2008-12-25
RU2007138584A (ru) 2009-04-27
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